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Pyrimidine amide derivatives and their salts

A technology for drugs and compounds, applied in the field of medicine, can solve the problems of cumbersome process, long time consumption, crystallization of preparations, etc., and achieve the effects of improving low solubility, reducing potential safety hazards and ensuring stability

Active Publication Date: 2018-03-13
JILIN SIHUAN PHARM CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Favipiravir has low water solubility, which has caused great limitations in preparation and administration, seriously affecting the clinical use effect
Furthermore, the poor water solubility will lead to crystallization of the preparation during storage and / or transportation, which will lead to hidden dangers in the safety of the clinical application of the drug
At present, many methods to improve the water solubility of favipiravir have been reported, such as making amorphous freeze-dried preparations after salt formation, but the process is cumbersome, time-consuming, and very inconvenient

Method used

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  • Pyrimidine amide derivatives and their salts
  • Pyrimidine amide derivatives and their salts
  • Pyrimidine amide derivatives and their salts

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Example 1 Preparation of 3-carbamoyl-5-fluoropyrazin-2-yl phosphate disodium (compound 1)

[0074] 1. Preparation of dibenzyl (3-carbamoyl-5-fluoropyrazin-2-yl) phosphate

[0075]

[0076] Add N,N-dimethylformamide (5mL) and 6-fluoro-3-hydroxypyrazine-2-carboxamide (200mg, 1.27mmol) into a 10mL two-necked flask, NaH (60%, 203mg, 5.08mmol) was added in batches, then stirred for 1 hour, and tetrabenzyl diphosphate (820mg, 1.52mmol) was added in batches. After the addition was complete, stirring was continued at room temperature for 3 hours. The solid was filtered and the crude product was purified by medium pressure preparation (mobile phase: CH 3 CN,H 2 O,1%NH 4 HCO 3 ), the fractions were collected and freeze-dried to obtain 192 mg of the product (36% yield) as a yellow solid.

[0077] 2. Preparation of disodium 3-carbamoyl-5-fluoropyrazin-2-ylphosphate

[0078]

[0079] Add dibenzyl (3-carbamoyl-5-fluoropyrazin-2-yl) phosphate (192 mg, 0.46 mmol) and dichl...

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Abstract

The invention belongs to the technical field of medicine, particularly relates to a pyrimidine amide derivative shown in a general formula (I) (please see the general formula in the description) or a pharmaceutically-acceptable salt of the pyrimidine amide derivative, a preparation method of the compounds, a pharmaceutical preparation and pharmaceutical composition containing the compounds and application of the compounds in preparation of medicine for treating and / or preventing virus infection, wherein X is defined in the description.

Description

technical field [0001] The present invention belongs to the technical field of medicine, and specifically relates to pyrimidine amide derivatives or pharmaceutically acceptable salts thereof, preparation methods of these compounds, pharmaceutical preparations and pharmaceutical compositions containing these compounds, and the preparation of these compounds for the treatment and / or prevention of viruses Use in medicine for infections. Background technique [0002] Influenza is an acute viral respiratory infectious disease caused by influenza virus, which seriously endangers human health. There have been several large-scale influenza epidemics in history, and the influenza epidemic in 1918 was the most serious, with more than 20 million deaths, and most of the deaths were young adults aged 15 to 45. Currently, the threat of influenza still exists. According to statistics, an average of 500,000 to 1,000,000 people worldwide die from influenza every year. [0003] At present, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/6509A61K31/661A61P31/16A61P31/22A61P31/12
CPCC07F9/650952Y02A50/30
Inventor 吴永谦
Owner JILIN SIHUAN PHARM CO LTD
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